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Effect of chemical enhancers in transdermal permeation of alfuzosin hydrochloride.

Prasanthi D, Lakshmi PK - ISRN Pharm (2012)

Bottom Line: All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug.Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr.Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, G. Pulla Reddy College of Pharmacy, Osmania University, Hyderabad, Andhra Pradesh 500 028, India.

ABSTRACT
The objective of the present study is to explore the efficient chemical penetration enhancer among the various enhancers available in overcoming the stratum corneum barrier in transdermal delivery of Alfuzosin hydrochloride (AH). The different enhancers were incorporated in 2% Carbopol gel which was selected as a control and evaluated by in vitro diffusion studies through dialysis membrane and permeation through the rat abdominal skin using Keshary-Chien diffusion cells. All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug. Among the various enhancers Transcutol 20% and tween-20 (2%) showed the highest cumulative amount (Q(24)) of 702.28 ± 6.97 μg/cm(2) and 702.74 ± 7.49 μg/cm(2), respectively. A flux rate of 31.08 ± 0.21 μg/cm(2)/hr by Transcutol 20% and 30.38 ± 0.18 μg/cm(2)/hr by tween-20 (2%) was obtained. Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr. The lowest skin content of 342.33 ± 5.30 μg/gm was seen with oleic acid 2.5%. Maximum enhancement of flux by 3.94-fold was obtained with transcutol 20%. Primary skin irritation studies were performed with rabbit. Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin. Among the different enhancers transcutol is efficient in enhancing transdermal delivery of AH.

No MeSH data available.


Related in: MedlinePlus

Histological slides of control (without any formulation), placebo (control gel), and CA12 (optimised chemical enhancer formulation).
© Copyright Policy - open-access
Related In: Results  -  Collection


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fig5: Histological slides of control (without any formulation), placebo (control gel), and CA12 (optimised chemical enhancer formulation).

Mentions: Histopathology studies of the optimized enhanced formulation (CA12) containing transcutol 20% and placebo gel (control without enhancer) were performed and compared with control (Figure 5) according to the protocol approved by institutional animal ethical committee. When compared with control H & E slides of placebo gel showed severe congestion, hemorrhage, and degeneration in dermis with moderate-to-severe inflammatory changes and edema in the epidermis. Slides of optimized formulation showed congestion, degeneration, and inflammatory cells predominantly mononuclear cell infiltration in the dermis.


Effect of chemical enhancers in transdermal permeation of alfuzosin hydrochloride.

Prasanthi D, Lakshmi PK - ISRN Pharm (2012)

Histological slides of control (without any formulation), placebo (control gel), and CA12 (optimised chemical enhancer formulation).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3539352&req=5

fig5: Histological slides of control (without any formulation), placebo (control gel), and CA12 (optimised chemical enhancer formulation).
Mentions: Histopathology studies of the optimized enhanced formulation (CA12) containing transcutol 20% and placebo gel (control without enhancer) were performed and compared with control (Figure 5) according to the protocol approved by institutional animal ethical committee. When compared with control H & E slides of placebo gel showed severe congestion, hemorrhage, and degeneration in dermis with moderate-to-severe inflammatory changes and edema in the epidermis. Slides of optimized formulation showed congestion, degeneration, and inflammatory cells predominantly mononuclear cell infiltration in the dermis.

Bottom Line: All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug.Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr.Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, G. Pulla Reddy College of Pharmacy, Osmania University, Hyderabad, Andhra Pradesh 500 028, India.

ABSTRACT
The objective of the present study is to explore the efficient chemical penetration enhancer among the various enhancers available in overcoming the stratum corneum barrier in transdermal delivery of Alfuzosin hydrochloride (AH). The different enhancers were incorporated in 2% Carbopol gel which was selected as a control and evaluated by in vitro diffusion studies through dialysis membrane and permeation through the rat abdominal skin using Keshary-Chien diffusion cells. All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug. Among the various enhancers Transcutol 20% and tween-20 (2%) showed the highest cumulative amount (Q(24)) of 702.28 ± 6.97 μg/cm(2) and 702.74 ± 7.49 μg/cm(2), respectively. A flux rate of 31.08 ± 0.21 μg/cm(2)/hr by Transcutol 20% and 30.38 ± 0.18 μg/cm(2)/hr by tween-20 (2%) was obtained. Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr. The lowest skin content of 342.33 ± 5.30 μg/gm was seen with oleic acid 2.5%. Maximum enhancement of flux by 3.94-fold was obtained with transcutol 20%. Primary skin irritation studies were performed with rabbit. Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin. Among the different enhancers transcutol is efficient in enhancing transdermal delivery of AH.

No MeSH data available.


Related in: MedlinePlus